In vitro inhibitory effects of Daphne oleoides ssp oleoides on inflammatory cytokines and activity-guided isolation of active constituents

Aerial parts of Daphne oleoides Schreber ssp, oleoides (Thymelaeaceae) are used to treat rheumatoid arthritis and lumbago in Turkish folk medicine. In order to evaluate folkloric utilization, in vitro inhibitory effects of th e ethyl acetate extract and fractions obtained from this extract on interle ukin 1 (IL-1 alpha, IL-1 beta) and tumour necrosis factor (TNF-alpha) biosy nthesis were studied, Through chemical isolation techniques and activity-gu ided fractionation process, seventeen compounds were isolated and their str uctures were elucidated (numbered 1-17). Diterpenoids genkwadaphnin (3) and 1,2-dehydrodaphnetoxin (6) and a coumarin derivative daphnetin (9) showed potent inhibitory activity and were found to be the main active ingredients . Furthermore, gnidilatin (4), gnidilatin-20 palmitate (5), genkwadaphnin-2 0-palmitate (7) and gnidicin-20-palmitate (8), having diterpenoid structure , and eudesmine (12), wikstromol (13) and matairesinol (14), having lignan structure, were determined to possess moderate inhibitory activity and may have a contributory role in the effect of the remedy. (C) 2001 Academic Pre ss.